[18F]MK-9470, a positron emission tomography (PET) tracer for in vivo human PET brain imaging of the cannabinoid-1 receptor
…, B Connolly, S Patel, S Krause… - Proceedings of the …, 2007 - National Acad Sciences
[ 18 F]MK-9470 is a selective, high-affinity, inverse agonist (human IC 50 , 0.7 nM) for the
cannabinoid CB1 receptor (CB1R) that has been developed for use in human brain imaging. …
cannabinoid CB1 receptor (CB1R) that has been developed for use in human brain imaging. …
Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S, 2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5 …
…, MT Goulet, WK Hagmann, LS Lin… - … of Pharmacology and …, 2007 - ASPET
The cannabinoid-1 receptor (CB1R) has been implicated in the control of energy balance.
To explore the pharmacological utility of CB1R inhibition for the treatment of obesity, we …
To explore the pharmacological utility of CB1R inhibition for the treatment of obesity, we …
[PDF][PDF] Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity
…, T Jian, M Jiang, Y Kan, TM Kelly, J Kosinski, LS Lin… - Cell metabolism, 2010 - cell.com
Bombesin receptor subtype 3 (BRS-3) is a G protein coupled receptor whose natural ligand
is unknown. We developed potent, selective agonist (Bag-1, Bag-2) and antagonist (Bantag-…
is unknown. We developed potent, selective agonist (Bag-1, Bag-2) and antagonist (Bantag-…
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a Novel …
LS Lin, TJ Lanza, JP Jewell, P Liu… - Journal of medicinal …, 2006 - ACS Publications
The discovery of novel acyclic amide cannabinoid-1 receptor inverse agonists is described.
They are potent, selective, orally bioavailable, and active in rodent models of food intake and …
They are potent, selective, orally bioavailable, and active in rodent models of food intake and …
Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques
…, JP Jewell, T Lanza Jr, LS Lin… - Journal of mass …, 2003 - Wiley Online Library
Metabolic activation of drug candidates to electrophilic reactive metabolites that can covalently
modify cellular macromolecules may result in acute and/or idiosyncratic immune system‐…
modify cellular macromolecules may result in acute and/or idiosyncratic immune system‐…
Discovery of MK-5046, a potent, selective bombesin receptor subtype-3 agonist for the treatment of obesity
…, RP Nargund, MJ Wyvratt, LS Lin - ACS Medicinal …, 2011 - ACS Publications
We report the development and characterization of compound 22 (MK-5046), a potent,
selective small molecule agonist of BRS-3 (bombesin receptor subtype-3). In pharmacological …
selective small molecule agonist of BRS-3 (bombesin receptor subtype-3). In pharmacological …
A facile microwave-assisted palladium-catalyzed cyanation of aryl chlorides
HR Chobanian, BP Fors, LS Lin - Tetrahedron letters, 2006 - Elsevier
We report an efficient method for the preparation of aryl nitriles from aryl chlorides under
either microwave assisted or thermal conditions. A catalyst system comprising tris(…
either microwave assisted or thermal conditions. A catalyst system comprising tris(…
Discovery of MK-4409, a novel oxazole FAAH inhibitor for the treatment of inflammatory and neuropathic pain
…, RP Nargund, MJ Wyvratt, LS Lin… - ACS Medicinal …, 2014 - ACS Publications
We report herein the identification of MK-4409, a potent and selective fatty acid amide
hydrolase (FAAH) inhibitor. Starting from a high throughput screening (HTS) hit, medicinal …
hydrolase (FAAH) inhibitor. Starting from a high throughput screening (HTS) hit, medicinal …
Deprotection of N-tert-butoxycarbonyl (Boc) groups in the presence of tert-butyl esters
LS Lin, T Lanza Jr, SE de Laszlo, Q Truong… - Tetrahedron …, 2000 - Elsevier
Deprotection of Boc groups in the presence of tert-butyl esters was achieved by using
concentrated H 2 SO 4 (1.5–3.0 equiv.) in tBuOAc or MeSO 3 H (1.5–3.0 equiv.) in tBuOAc:CH 2 Cl …
concentrated H 2 SO 4 (1.5–3.0 equiv.) in tBuOAc or MeSO 3 H (1.5–3.0 equiv.) in tBuOAc:CH 2 Cl …
Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist
…, I Sebhat, LS Lin, J Dragovic, KA Lyons, S Craw… - … of Pharmacology and …, 2011 - ASPET
Bombesin receptor subtype-3 (BRS-3) is an orphan G protein-coupled receptor implicated
in the regulation of energy homeostasis. Here, we report the biologic effects of a highly …
in the regulation of energy homeostasis. Here, we report the biologic effects of a highly …